JP2017531663A - 14員ケトライドならびにそれらの調製および使用の方法 - Google Patents
14員ケトライドならびにそれらの調製および使用の方法 Download PDFInfo
- Publication number
- JP2017531663A JP2017531663A JP2017519264A JP2017519264A JP2017531663A JP 2017531663 A JP2017531663 A JP 2017531663A JP 2017519264 A JP2017519264 A JP 2017519264A JP 2017519264 A JP2017519264 A JP 2017519264A JP 2017531663 A JP2017531663 A JP 2017531663A
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- certain embodiments
- hydrogen
- formula
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Tropical Medicine & Parasitology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462061571P | 2014-10-08 | 2014-10-08 | |
| US62/061,571 | 2014-10-08 | ||
| PCT/US2015/054700 WO2016057798A1 (en) | 2014-10-08 | 2015-10-08 | 14-membered ketolides and methods of their preparation and use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017531663A true JP2017531663A (ja) | 2017-10-26 |
| JP2017531663A5 JP2017531663A5 (enExample) | 2018-11-15 |
Family
ID=55653777
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017519264A Pending JP2017531663A (ja) | 2014-10-08 | 2015-10-08 | 14員ケトライドならびにそれらの調製および使用の方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10633407B2 (enExample) |
| EP (1) | EP3211997A4 (enExample) |
| JP (1) | JP2017531663A (enExample) |
| CN (1) | CN106998685A (enExample) |
| CA (1) | CA2963815A1 (enExample) |
| HK (1) | HK1242920A1 (enExample) |
| WO (1) | WO2016057798A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4095146A1 (en) | 2013-04-04 | 2022-11-30 | President And Fellows Of Harvard College | Macrolides and methods of their preparation and use |
| JP2017531663A (ja) | 2014-10-08 | 2017-10-26 | プレジデント アンド フェローズ オブ ハーバード カレッジ | 14員ケトライドならびにそれらの調製および使用の方法 |
| WO2016154591A1 (en) | 2015-03-25 | 2016-09-29 | President And Fellows Of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
| US11673910B2 (en) | 2017-04-28 | 2023-06-13 | Zikani Therapeutics, Inc. | Macrolides with modified desosamine sugars and uses thereof |
| IL283185B2 (en) | 2018-11-19 | 2024-06-01 | Zikani Therapeutics Inc | Macrolides with 13 members converted to C10-cyclic and their uses |
| AU2019385333B2 (en) | 2018-11-19 | 2025-04-17 | President And Fellows Of Harvard College | C10-alkylene substituted 13-membered macrolides and uses thereof |
| IL303173A (en) * | 2023-05-23 | 2024-12-01 | Yeda Res & Dev | Active macrolide antibiotic compounds against pathogens |
| WO2025228440A1 (zh) * | 2024-04-30 | 2025-11-06 | 苏州信诺维医药科技股份有限公司 | 大环内酯类化合物、其制备方法及其用途 |
Citations (13)
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| JP2002519032A (ja) * | 1998-06-29 | 2002-07-02 | バイオティカ テクノロジー リミティド | ポリケチドとその合成 |
| WO2004080391A2 (en) * | 2003-03-10 | 2004-09-23 | Optimer Pharmaceuticals, Inc. | Novel antibacterial agents |
| JP2005511752A (ja) * | 2001-12-05 | 2005-04-28 | オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド | 抗バクテリア剤として有効なエリスロマイシンの6−O−アシルケトーリド(ketolide)誘導体 |
| JP2008526808A (ja) * | 2005-01-12 | 2008-07-24 | アルファーマ エーピーエス | マクロライド |
| US20090170790A1 (en) * | 2004-10-25 | 2009-07-02 | Biswajit Das | Ketolide derivatives as antibacterial agents |
| JP2010501541A (ja) * | 2006-08-24 | 2010-01-21 | ウォックハート リサーチ センター | 抗菌活性を有する新規マクロライド及びケトライド |
| JP2011500834A (ja) * | 2007-10-25 | 2011-01-06 | センプラ ファーマスーティカルズ,インコーポレイテッド | マクロライド系抗菌剤の調製プロセス |
| US8063021B2 (en) * | 2002-01-17 | 2011-11-22 | Kosan Biosciences Incorporated | Ketolide anti-infective compounds |
| JP2013501757A (ja) * | 2009-08-13 | 2013-01-17 | バジリア ファルマスーチカ アーゲー | 新規マクロライド及びその使用 |
| JP2013527187A (ja) * | 2010-05-20 | 2013-06-27 | センプラ ファーマシューティカルズ,インコーポレイテッド | マクロライド類およびケトライド類ならびにその中間体を調製するための工程 |
| JP2013537198A (ja) * | 2010-09-10 | 2013-09-30 | センプラ ファーマシューティカルズ,インコーポレイテッド | 疾患治療のための水素結合形成フルオロケトライド |
| US8796474B1 (en) * | 2010-08-23 | 2014-08-05 | Rutgers, The State University Of New Jersey | Macrolide compounds and methods and intermediates useful for their preparation |
| WO2014165792A2 (en) * | 2013-04-04 | 2014-10-09 | President And Fellows Of Harvard College | Macrolides and methods of their preparation and use |
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| ZA859575B (en) | 1984-12-21 | 1986-08-27 | Hoffmann La Roche | Oxetanones |
| FR2718450B1 (fr) * | 1994-04-08 | 1997-01-10 | Roussel Uclaf | Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments. |
| JP3652394B2 (ja) | 1995-01-27 | 2005-05-25 | 高砂香料工業株式会社 | N−置換−7−アミノ−5−ヒドロキシ−3−オキソヘプタン酸誘導体およびその製造法 |
| HN1998000074A (es) | 1997-06-11 | 1999-01-08 | Pfizer Prod Inc | Derivados de macrolidos c-4 sustituidos |
| WO1999000125A1 (en) | 1997-06-27 | 1999-01-07 | Merck & Co., Inc. | 9a-aza-3-ketolides, compositions containing such compounds and methods of treatment |
| HN1998000159A (es) | 1997-10-29 | 1999-02-09 | Monsanto Co | Derivados de 9- amino - 3 ceto eritromicina |
| FR2785612A1 (fr) | 1998-11-10 | 2000-05-12 | Hoechst Marion Roussel Inc | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
| US6262030B1 (en) | 1998-11-03 | 2001-07-17 | Pfizer Inc. | Erythromycin derivatives |
| US6590083B1 (en) | 1999-04-16 | 2003-07-08 | Ortho-Mcneil Pharmaceutical, Inc. | Ketolide antibacterials |
| US6939861B2 (en) * | 1999-04-16 | 2005-09-06 | Kosan Biosciences, Inc. | Amido macrolides |
| US6399582B1 (en) * | 1999-04-16 | 2002-06-04 | Ortho-Mcneil Pharmaceutical, Inc. | Ketolide antibacterials |
| HRP990116B1 (en) | 1999-04-20 | 2007-10-31 | GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. | NOVEL 8a AND 9a- 15-MEMBERED LACTAMES |
| EE200100613A (et) * | 1999-05-24 | 2003-02-17 | Pfizer Products Inc. | 13-metüülerütromütsiini derivaadid |
| AU6316400A (en) * | 1999-08-06 | 2001-03-05 | Taisho Pharmaceutical Co., Ltd. | Erythromycin a derivatives |
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| ATE243703T1 (de) | 2000-01-27 | 2003-07-15 | Pfizer Prod Inc | Antibiotische azalid-zusammensetzungen |
| JP4596591B2 (ja) | 2000-03-09 | 2010-12-08 | 塩野義製薬株式会社 | 8a−オキサホモエリスロマイシン誘導体、製造方法、合成中間体および医薬組成物 |
| US6440942B1 (en) | 2000-12-22 | 2002-08-27 | Enanta Pharmaceuticals, Inc. | 14-membered macrolides derived from leucomycins |
| RU2330069C2 (ru) | 2002-11-29 | 2008-07-27 | Мершан Корпорейшн | Способ получения макролидного соединения и штаммы streptomyces sp., mortierella sp. и micromonosporaceae |
| JPWO2004065346A1 (ja) | 2003-01-21 | 2006-05-18 | 住友化学株式会社 | (−)−テトラヒドロリプスタチンおよびその中間体の製造方法 |
| HRP20030381B1 (en) | 2003-05-14 | 2007-05-31 | GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. | 3-DECLADINOZYL 9a-N-CARBAMOYL AND 9a-N-THIOCARBAMOYL DERIVATIVES 9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERYTHROMICYNE A |
| US7276487B2 (en) | 2003-09-23 | 2007-10-02 | Enanta Pharmaceuticals, Inc. | 9a, 11-3C-bicyclic 9a-azalide derivatives |
| WO2006080954A1 (en) * | 2004-07-28 | 2006-08-03 | Ranbaxy Laboratories Limited | Ketolide derivatives as antibacterial agents |
| US7767797B1 (en) | 2004-09-30 | 2010-08-03 | Synovo Gmbh | Macrocyclic compounds and methods of use thereof |
| US20060096158A1 (en) | 2004-11-08 | 2006-05-11 | Robinson J M | Lactones as new oxygenate fuel additives, fuels based thereon and methods for using same |
| CN101103039A (zh) * | 2005-01-12 | 2008-01-09 | 阿尔法马股份公司 | 作为抗菌剂的红霉素衍生物 |
| DE602006015919D1 (de) | 2005-01-13 | 2010-09-16 | Glaxosmithkline Zagreb | Makrolide mit entzündungshemmender wirkung |
| JP2008540503A (ja) | 2005-05-10 | 2008-11-20 | グラクソスミスクライン・イストラジヴァッキ・センタル・ザグレブ・ドルズバ・ゼー・オメイェノ・オドゴヴォルノスティオ | 細菌感染症の処置に有用なエーテル結合マクロライド |
| RU2008106915A (ru) | 2005-07-26 | 2009-09-10 | Меркле Гмбх (De) | Макролидные конъюгаты пирролиновых и индолизиновых соединений |
| CN101282967B (zh) | 2005-10-13 | 2011-01-26 | 卫材R&D管理有限公司 | 普拉二烯内酯b和普拉二烯内酯d的全合成 |
| WO2007091393A1 (ja) | 2006-02-07 | 2007-08-16 | Taisho Pharmaceutical Co., Ltd. | 10a-アザライド化合物 |
| MX2009009074A (es) * | 2007-03-13 | 2009-09-28 | Pfizer Prod Inc | Macrolidos basados en eritromicina. |
| US20090209547A1 (en) | 2008-02-15 | 2009-08-20 | In Jong Kim | C-8 halogenated macrolides |
| KR100980379B1 (ko) | 2008-04-02 | 2010-09-06 | 주식회사 파마코스텍 | 광학활성을 갖는 5-히드록시-3-옥소헵타노에이트 유도체의제조방법 |
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| CN107854477A (zh) | 2008-10-24 | 2018-03-30 | 森普拉制药公司 | 使用含三唑的大环内酯治疗抗性疾病的方法 |
| US9480679B2 (en) | 2009-09-10 | 2016-11-01 | Cempra Pharmaceuticals, Inc. | Methods for treating malaria, tuberculosis and MAC diseases |
| WO2011112864A1 (en) | 2010-03-10 | 2011-09-15 | Cempra Pharmaceuticals, Inc. | Parenteral formulations of macrolide antibiotics |
| HRP20160168T1 (hr) | 2010-03-22 | 2016-03-25 | Cempra Pharmaceuticals Inc | Kristalne forme makrolida i njihova uporaba |
| WO2011131749A1 (en) * | 2010-04-23 | 2011-10-27 | Glaxo Group Limited | New 14 and 15 membered macrolides for the treatment of neutrophil dominated inflammatory diseases |
| EP2588084B1 (en) | 2010-07-01 | 2023-11-22 | Elanco Tiergesundheit AG | Antibiotic compositions comprising tulathromycin |
| WO2012016186A1 (en) | 2010-07-29 | 2012-02-02 | President And Fellows Of Harvard College | Macrocyclic kinase inhibitors and uses thereof |
| US9145436B2 (en) | 2010-10-10 | 2015-09-29 | Michael W. Burnet | Anti-inflammatory macrolides |
| EP2688900B1 (en) * | 2011-03-22 | 2016-09-28 | Wockhardt Limited | Process for preparation of ketolide compounds |
| CN102690297A (zh) | 2011-03-22 | 2012-09-26 | 连云港海康生物科技有限公司 | 一种壳寡糖季铵盐及其合成方法 |
| CA2843853A1 (en) * | 2011-07-01 | 2013-01-10 | President And Fellows Of Harvard College | Macrocyclic insulin-degrading enzyme (ide) inhibitors and uses thereof |
| WO2013148891A1 (en) | 2012-03-27 | 2013-10-03 | Cempra Pharmaceuticals, Inc. | Parenteral formulations for administering macrolide antibiotics |
| WO2014152326A1 (en) | 2013-03-14 | 2014-09-25 | Cempra Pharmaceuticals, Inc. | Methods for treating respiratory diseases and formulations therefor |
| AU2014233240B2 (en) | 2013-03-15 | 2018-08-09 | Cempra Pharmaceuticals, Inc. | Convergent processes for preparing macrolide antibacterial agents |
| JP2017531663A (ja) | 2014-10-08 | 2017-10-26 | プレジデント アンド フェローズ オブ ハーバード カレッジ | 14員ケトライドならびにそれらの調製および使用の方法 |
| EP3277701A4 (en) | 2015-03-25 | 2019-03-06 | President and Fellows of Harvard College | SYNTHESIS OF DESOSAMINES |
| WO2016154591A1 (en) | 2015-03-25 | 2016-09-29 | President And Fellows Of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
-
2015
- 2015-10-08 JP JP2017519264A patent/JP2017531663A/ja active Pending
- 2015-10-08 WO PCT/US2015/054700 patent/WO2016057798A1/en not_active Ceased
- 2015-10-08 EP EP15848340.4A patent/EP3211997A4/en not_active Withdrawn
- 2015-10-08 HK HK18102636.6A patent/HK1242920A1/zh unknown
- 2015-10-08 CN CN201580066344.5A patent/CN106998685A/zh active Pending
- 2015-10-08 US US15/517,843 patent/US10633407B2/en active Active
- 2015-10-08 CA CA2963815A patent/CA2963815A1/en not_active Abandoned
-
2020
- 2020-04-08 US US16/843,259 patent/US11466046B2/en active Active
-
2022
- 2022-07-25 US US17/872,769 patent/US20230109357A1/en not_active Abandoned
Patent Citations (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002519032A (ja) * | 1998-06-29 | 2002-07-02 | バイオティカ テクノロジー リミティド | ポリケチドとその合成 |
| JP2005511752A (ja) * | 2001-12-05 | 2005-04-28 | オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド | 抗バクテリア剤として有効なエリスロマイシンの6−O−アシルケトーリド(ketolide)誘導体 |
| US8063021B2 (en) * | 2002-01-17 | 2011-11-22 | Kosan Biosciences Incorporated | Ketolide anti-infective compounds |
| WO2004080391A2 (en) * | 2003-03-10 | 2004-09-23 | Optimer Pharmaceuticals, Inc. | Novel antibacterial agents |
| US20090170790A1 (en) * | 2004-10-25 | 2009-07-02 | Biswajit Das | Ketolide derivatives as antibacterial agents |
| JP2008526808A (ja) * | 2005-01-12 | 2008-07-24 | アルファーマ エーピーエス | マクロライド |
| JP2010501541A (ja) * | 2006-08-24 | 2010-01-21 | ウォックハート リサーチ センター | 抗菌活性を有する新規マクロライド及びケトライド |
| JP2011500834A (ja) * | 2007-10-25 | 2011-01-06 | センプラ ファーマスーティカルズ,インコーポレイテッド | マクロライド系抗菌剤の調製プロセス |
| JP2013501757A (ja) * | 2009-08-13 | 2013-01-17 | バジリア ファルマスーチカ アーゲー | 新規マクロライド及びその使用 |
| JP2013527187A (ja) * | 2010-05-20 | 2013-06-27 | センプラ ファーマシューティカルズ,インコーポレイテッド | マクロライド類およびケトライド類ならびにその中間体を調製するための工程 |
| US8796474B1 (en) * | 2010-08-23 | 2014-08-05 | Rutgers, The State University Of New Jersey | Macrolide compounds and methods and intermediates useful for their preparation |
| JP2013537198A (ja) * | 2010-09-10 | 2013-09-30 | センプラ ファーマシューティカルズ,インコーポレイテッド | 疾患治療のための水素結合形成フルオロケトライド |
| WO2014165792A2 (en) * | 2013-04-04 | 2014-10-09 | President And Fellows Of Harvard College | Macrolides and methods of their preparation and use |
Also Published As
| Publication number | Publication date |
|---|---|
| CN106998685A (zh) | 2017-08-01 |
| CA2963815A1 (en) | 2016-04-14 |
| HK1242920A1 (zh) | 2018-07-06 |
| EP3211997A1 (en) | 2017-09-06 |
| US11466046B2 (en) | 2022-10-11 |
| US10633407B2 (en) | 2020-04-28 |
| WO2016057798A1 (en) | 2016-04-14 |
| US20200361980A1 (en) | 2020-11-19 |
| EP3211997A4 (en) | 2018-10-24 |
| US20170305953A1 (en) | 2017-10-26 |
| US20230109357A1 (en) | 2023-04-06 |
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